A kind of sodium alginate-based pH-responsive drug microcapsules and preparation method thereof

A technology of sodium alginate and microcapsules, which is applied in microcapsules, capsule delivery, pharmaceutical formulations, etc. It can solve the problems of unstable drug release performance, poor mechanical properties of wall materials, and large particle size of microcapsules, so as to improve hydrophilicity non-toxic, smooth surface and evenly distributed effect

Inactive Publication Date: 2017-12-12
HEBEI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The purpose of the present invention is to provide a sodium alginate-based pH-responsive drug microcapsule and its preparation method, to solve the problem of large particle size, uneven distribution, low encapsulation efficiency, poor mechanical properties of wall materials and problems of existing microcapsules. Unstable drug release performance and other issues

Method used

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  • A kind of sodium alginate-based pH-responsive drug microcapsules and preparation method thereof
  • A kind of sodium alginate-based pH-responsive drug microcapsules and preparation method thereof
  • A kind of sodium alginate-based pH-responsive drug microcapsules and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] (1) Take 25mL of ethyl acetate, add 10g of methyl methacrylate, 0.8g of cross-linking agent 1,4-butanediol dimethacrylate and 1.5g of felodipine in turn to the ethyl acetate, stir well, get oily phase;

[0045] (2) Take 300mL of water, add 4g of sodium alginate and 0.08g of surfactant poloxamer-188 into the water, stir well to obtain the water phase;

[0046] (3) Add the oil phase to the water phase, and use a high-speed shear emulsifier to shear and emulsify for 9 minutes at a shear rate of 8000 r / min to obtain an oil / water emulsion;

[0047] (4) Put the prepared oil / water emulsion into the mixture equipped with agitator, constant pressure dropping funnel, N 2 four-necked flask with catheter and thermometer, in N 2 Stir mechanically under the atmosphere, heat to 60°C, slowly add 150mL aqueous solution containing cerium ammonium nitrate with a concentration of 0.0027g / mL (a solution obtained by dissolving 0.4g of cerium ammonium nitrate in 150mL of water); keep the te...

Embodiment 2

[0049] (1) Take 23mL of ethyl acetate, add 8g of ethyl methacrylate, 0.6g of cross-linking agent 1,4-butanediol dimethacrylate and 1.0g of felodipine in turn to the ethyl acetate, stir well, get oily phase;

[0050] (2) Take 225 mL of water, add 3 g of sodium alginate and 0.06 g of surfactant poloxamer-188 into the water, stir well to obtain the water phase;

[0051] (3) Add the oil phase to the water phase, and use a high-speed shear emulsifier to emulsify for 9 minutes at a shear rate of 8000r / min to obtain an oil / water emulsion;

[0052] (4) Put the prepared oil / water emulsion into the mixture equipped with agitator, constant pressure dropping funnel, N 2 four-necked flask with catheter and thermometer, in N 2 Stir mechanically under the atmosphere, heat to 60°C, slowly add 113mL aqueous solution containing cerium ammonium nitrate with a concentration of 0.0027g / mL (a solution obtained by dissolving 0.3g of cerium ammonium nitrate in 113mL of water); keep the temperature ...

Embodiment 3

[0054] (1) Take 30 mL of ethyl acetate, add 12 g of butyl methacrylate, 1.0 g of cross-linking agent 1,4-butanediol dimethacrylate and 2.0 g of felodipine in sequence, and stir well , to get the oil phase;

[0055] (2) Take 375mL of water, add 5g of sodium alginate and 0.1g of surfactant poloxamer-188 into the water, stir well to obtain the water phase;

[0056] (3) Add the oil phase to the water phase, and use a high-speed shear emulsifier to shear and emulsify for 9 minutes at a shear rate of 8000 r / min to obtain an oil / water emulsion;

[0057] (4) Put the prepared oil / water emulsion into the mixture equipped with agitator, constant pressure dropping funnel, N 2 four-necked flask with catheter and thermometer, in N 2 Stir mechanically under the atmosphere, heat to 60°C, slowly add dropwise 188mL aqueous solution containing 0.0027g / mL cerium ammonium nitrate (a solution obtained by dissolving 0.5g cerium ammonium nitrate in 188mL water); keep the temperature constant, react...

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Abstract

The invention discloses a sodium alginate-based pH-responsive drug microcapsule, which comprises the following components in parts by weight: 8-12 parts of a hydrophobic vinyl monomer, 0.6-1 part of a cross-linking agent containing a double bond, and a hydrophobic drug 1-2 parts, 3-5 parts of sodium alginate monomer, 0.06-0.1 parts of hydrophilic surfactant, 0.3-0.5 parts of initiator, 20-30 parts of oil-soluble drug solvent and 338-563 parts of water. The preparation method includes: a) weighing each component; b) dissolving hydrophobic vinyl monomer, double bond-containing cross-linking agent and drug in an oil-soluble drug solvent to obtain an oil phase; c) dissolving sodium alginate 1. The surfactant is dissolved in water to obtain a water phase; d) Add the oil phase to the water phase and emulsify to obtain an oil / water emulsion; e) After the oil / water emulsion is heated up, add an aqueous solution of the initiator dropwise, and after the reaction, centrifuge , washing and drying to obtain microcapsules. The preparation method provided by the invention is simple, easy to operate and has good reproducibility, and the prepared microcapsules have small particle size, uniform distribution, high encapsulation rate, good wall material mechanical properties and stable drug release performance.

Description

technical field [0001] The invention relates to a pharmaceutical dosage form and a preparation method thereof, in particular to a sodium alginate-based pH-responsive drug microcapsule and a preparation method thereof. Background technique [0002] Microcapsule refers to the use of natural or synthetic polymer capsule wall materials to coat solid, liquid, or even gaseous micro-capsule core substances to form a semi-permeable or sealed capsule with a diameter of 1-5000μm. capsule. The outstanding feature of sodium alginate (SA)-based drug microcapsules is good pH responsiveness, that is, the microcapsules are stable in acidic gastric juice with low pH, and the drug is hardly released, while in alkaline intestinal juice with high pH, The swelling property of the wall material is increased, and the release rate of the drug is increased, which can protect the drug from being damaged by gastric acid, and can be made into an intestinal-directed drug delivery preparation. In the p...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K45/00A61K31/4422A61K47/36
Inventor 安朴英窦圣博崔海阳王金芳巴信武
Owner HEBEI UNIVERSITY
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